A novel process for the preparation of teriflunomide

The present invention provides a process for the preparation of Teriflunomide (Formula-I). The present invention describes the synthesis of Teriflunomide without isolating the intermediate Leflunomide. Teriflunomide is prepared from 5-Methyl isoxazole-4-carboxylic acid by converting to its acid chlo...

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Bibliographische Detailangaben
Hauptverfasser:	Shanmughasamy, Rajmahendra, Babu, Jithendra R, Palle, Venkata Raghavendracharyulu, Kaliappan, Mariappan, Bhat, Ramakrishna Parameshwar
Format:	Patent
Sprache:	eng
Schlagworte:	ACYCLIC OR CARBOCYCLIC COMPOUNDS CHEMISTRY METALLURGY ORGANIC CHEMISTRY
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Beschreibung
Zusammenfassung:	The present invention provides a process for the preparation of Teriflunomide (Formula-I). The present invention describes the synthesis of Teriflunomide without isolating the intermediate Leflunomide. Teriflunomide is prepared from 5-Methyl isoxazole-4-carboxylic acid by converting to its acid chloride and coupling with 4-trifluoromethyl aniline to obtain Leflunomide (which is not isolated) followed by ring opening reaction using aq. Sodium Hydroxide to form Teriflunomide. In other words, the process is telescoped from 5- methylisoxazole-4-carbonyl chloride.